Progress in Medicinal Chemistry ( Volume 56 )

Publication series ：Volume 56

Author： Witty   David R.;Cox   Brian  

Publisher： Elsevier Science‎

Publication year： 2017

E-ISBN: 9780444639431

P-ISBN(Paperback): 9780444639394

Subject： R914 pharmaceutical chemistry

Keyword： 有机化学,化学,临床医学,动物学,生物化学,药学

Language： ENG

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Description

Progress in Medicinal Chemistry, Volume 56 provides a review of eclectic developments in medicinal chemistry. This volume includes chapters covering recent advances in cancer therapeutics, fluorine in medicinal chemistry, a perspective on the next generation of antibacterial agents derived by manipulation of natural products, a potential new era for Chagas Disease drug discovery, and imaging in drug development. Specific chapters cover timely topics, such as the development of LRRK2 inhibitors for the treatment of Parkinson's, and recent discoveries and developments in TRPA1 modulators.

Users will find a comprehensive resource on the topic of medicinal chemistry that also discusses avenues for the acceleration of drug discovery programs.

  • Extended, timely reviews of topics in medicinal chemistry
  • Contains targets and technologies relevant to the discovery of tomorrow’s drugs
  • Presents analyses of successful drug discovery programs

Chapter

Front Cover

Progress in Medicinal Chemistry

Copyright

Contents

Contributors

Preface

Chapter One: Enabling Chemistry Technologies and Parallel Synthesis-Accelerators of Drug Discovery Programmes

1. Introduction

2. The Evolution of Flow-Based Approaches to Synthesis

3. Use of High-Temperature Chemistries

4. Use of Photochemical and Electrochemical Reactions

5. Use of Hazardous Gases (e.g. Diazomethane) in Flow

6. Library Design Tools and Processes

7. Use of Flow Chemistry for Library Synthesis

8. Summary and Future Perspectives

Acknowledgements

References

Chapter Two: Development of LRRK2 Inhibitors for the Treatment of Parkinson´s Disease

1. Introduction

2. LRRK2 Biology

2.1. Genetic Evidence for the Possible Role of LRRK2 in PD

2.2. Localisation and Function of LRRK2

3. Structural Biology of LRRK2

4. Overview of Selective Inhibitors of LRRK2

4.1. Diaminopyrimidines

4.2. Arylbenzamides

4.3. Indolinones

4.4. Indazoles

4.5. Cinnolines/Quinolines

4.6. Pyrrolopyrimidines

4.7. Thiophenes

4.8. Triazolopyridazines

5. Conclusion

References

Chapter Three: Recent Progress in the Discovery and Development of TRPA1 Modulators

1. TRPA1: An Introduction

2. Validation as a Target for Drug Discovery

2.1. TRPA1 Modulators for Inflammatory and Neuropathic Pain

2.2. TRPA1 Modulators for Respiratory Disorders

2.3. TRPA1 Modulators as Migraine Therapeutics

2.4. TRPA1 Modulators: Additional Potential Therapeutic Indications

2.4.1. TRPA1 in GI Tract Indications

2.4.2. TRPA1 in Urogenital Indications

2.4.3. TRPA1 in Cerebral Vascular Function and Cardiovascular Indications

2.4.4. TRPA1 in CNS Indications

2.4.5. TRPA1 in Itch

2.5. Safety Considerations

3. Medicinal Chemistry and Clinical Status of TRPA1 Modulators

4. Recent Structural Insights

5. Conclusions and Outlook

References

Chapter Four: Small Molecule Inhibition of Interleukin-1 Receptor-Associated Kinase 4 (IRAK4)

1. Introduction

1.1. IRAK4 and TLR/IL-1R Signalling Pathways

1.2. IRAK4 Structure and Function

1.3. Therapeutic Potential of IRAK4 Inhibition

1.3.1. Autoimmune/Inflammatory Diseases

1.3.2. Oncology

1.3.3. Neurological Disorders

2. Small Molecule IRAK4 Inhibitor Discovery

2.1. Ares Trading S.A.

2.2. Astellas Pharma Inc.

2.3. Aurigene Discovery Technologies Limited

2.4. Bayer Pharma

2.5. Biogen

2.6. Bristol-Meyers Squibb

2.7. Hoffmann-La Roche

2.8. Ligand Pharmaceuticals

2.9. Merck Serono/KGaA

2.10. Merck Sharp and Dohme Corp.

2.11. Nimbus Therapeutics

2.12. Pfizer, Inc.

2.13. Tularik/Amgen

2.14. Takeda Pharmaceutical Company Limited

3. Summary of Clinical Status

4. Conclusion

References

Index

Back Cover

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